scholarly journals Synthesis of Alamandine Glycoside Analogues as New Drug Candidates to Antagonize the MrgD Receptor for Pain Relief

2021 ◽  
Author(s):  
Wafaa Alabsi ◽  
Timothy Jaynes ◽  
Tariq Alqahtani ◽  
Lajos Szabo ◽  
Daekyu Sun ◽  
...  
Keyword(s):  
Molecular Weight ◽  
Chemical Composition ◽  
Pain Relief ◽  
Cell Lines ◽  
Receptor Expression ◽  
Human Cell Lines ◽  
Hek 293 ◽  
Drug Candidates ◽  
C Terminus ◽  
Analytical Hplc

Abstract Two series of putatively brain-penetrant alamandine glycosides have been prepared for screening against the MrgD receptor. One series has retained the first 6 residues of the alamandine sequence (ARVYIH), replacing the terminal proline (P) with serine (S) glycosides at the C-terminus. In the second series, the alteration of the steric bulk was performed by changing the initial alanine (A) residue with glycine (G); D-alanine (a); nor-valine (norV); D-nor-valine (D-norV); valine (V); and D-nor-valine (v) with keeping the serine-beta-D-glucoside (S-Glc) at the C-terminus. All the peptides and glycopeptides were synthesized as their C-terminal amide. The purity of native alamandine and its eleven selected derivatives was confirmed using analytical HPLC. Also, the molecular weight and chemical composition were confirmed using mass spectroscopy. The MrgD receptor expression was evaluated in rationally chosen human cell lines, A549 and HEK 293. Both cell lines showed the presence of the MrgD receptor around 35 kDa, as confirmed by western blot analysis. The effect of varying concentrations of some alamandine derivatives on cell viability was evaluated on HEK 293 and A549 cell lines.

Heterogeneity of Fcγ receptor expression on human cell lines

1983 ◽  
Vol 7 (2) ◽  
pp. 85-89 ◽  
Author(s):  
D.W. Hough ◽  
A. Narendran ◽  
N.D. Hall
Keyword(s):  
Cell Lines ◽  
Human Cell ◽  
Receptor Expression ◽  
Human Cell Lines ◽  
Fcγ Receptor

FindingNemo in OneDay: Ultra-Long ONT Library Preparation from Cell to Flowcell in One Day v1

2021 ◽  
Author(s):  
Inswasti Cahyani ◽  
John Tyson ◽  
Nadine Holmes ◽  
Josh Quick ◽  
Nicholas Loman ◽  
...  
Keyword(s):  
Molecular Weight ◽  
High Molecular Weight ◽  
Cell Lines ◽  
Human Cell ◽  
Human Cell Lines ◽  
Library Preparation ◽  
Dna Library ◽  
Oxford Nanopore ◽  
Working Day ◽  
Ultra High Molecular Weight

This protocol is focussed on the isolation of ultra-high molecular weight (UHMW) DNA, library preparation and clean up ready for sequencing on the Oxford Nanopore Technology (ONT) platforms, all within one working day. This protocol is optimised for human cell lines. Summary of the workflow:

scholarly journals Investigations on Anticancer Potentials by DNA Binding and Cytotoxicity Studies for Newly Synthesized and Characterized Imidazolidine and Thiazolidine-Based Isatin Derivatives

Molecules ◽  
2022 ◽  
Vol 27 (2) ◽  
pp. 354
Author(s):  
Nasima Arshad ◽  
Muhammad Ismail Mir ◽  
Fouzia Perveen ◽  
Aneela Javed ◽  
Memona Javaid ◽  
...  
Keyword(s):  
Dna Binding ◽  
Cell Lines ◽  
Liver Carcinoma ◽  
Hek 293 ◽  
Drug Candidates ◽  
293 Cells ◽  
Cytotoxicity Studies ◽  
Experimental Findings ◽  
Isatin Derivatives ◽  
Mcf 7

Imidazolidine and thiazolidine-based isatin derivatives (IST-01–04) were synthesized, characterized, and tested for their interactions with ds-DNA. Theoretical and experimental findings showed good compatibility and indicated compound–DNA binding by mixed mode of interactions. The evaluated binding parameters, i.e., binding constant (Kb), free energy change (ΔG), and binding site sizes (n), inferred comparatively greater and more spontaneous binding interactions of IST-02 and then IST-04 with the DNA, among all compounds tested under physiological pH and temperature (7.4, 37 °C). The cytotoxic activity of all compounds was assessed against HeLa (cervical carcinoma), MCF-7 (breast carcinoma), and HuH-7 (liver carcinoma), as well as normal HEK-293 (human embryonic kidney) cell lines. Among all compounds, IST-02 and 04 were found to be cytotoxic against HuH-7 cell lines with percentage cell toxicity of 75% and 66%, respectively, at 500 ng/µL dosage. Moreover, HEK-293 cells exhibit tolerance to the increasing drug concentration, suggesting these two compounds are less cytotoxic against normal cell lines compared to cancer cell lines. Hence, both DNA binding and cytotoxicity studies proved imidazolidine (IST-02) and thiazolidine (IST-04)-based isatin derivatives as potent anticancer drug candidates among which imidazolidine (IST-02) is comparatively the more promising.

scholarly journals Screening and testing for a suitable untransfected cell line for SARS-CoV-2 studies

2020 ◽  
Author(s):  
Claudia Pommerenke ◽  
Ulfert Rand ◽  
Cord C. Uphoff ◽  
Stefan Nagel ◽  
Margarete Zaborski ◽  
...  
Keyword(s):  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cell ◽  
Viral Entry ◽  
Cancer Cell Line ◽  
Receptor Expression ◽  
Host Factors ◽  
Human Cell Lines ◽  
Infection Models

AbstractAt present, the novel pandemic coronavirus SARS-CoV-2 is a major global threat to human health and hence demands united research activities at different levels. Finding appropriate cell systems for drug screening and testing molecular interactions of the virus with the host cell is mandatory for drug development and understanding the mechanisms of viral entry and replication. For this, we selected human cell lines represented in the Cancer Cell Line Encyclopedia (CCLE) based on RNA-seq data determined transcript levels of ACE2 and TMPRSS2, two membrane proteins that have been identified to aid SARS-CoV-2 entry into the host cell. mRNA and protein expression of these host factors were verified via RQ-PCR and western blot. We then tested permissiveness of these cell lines towards SARS-CoV-2 infection, cytopathic effect, and viral replication finding limited correlation between receptor expression and infectability. One of the candidate cancer cell lines, the human colon cancer cell line CL-14, tested positive for SARS-CoV-2 infection. Our data argue that SARS-CoV-2 in vitro infection models need careful selection and validation since ACE2/TMPRSS2 receptor expression on its own does not guarantee permissiveness to the virus.Author summaryIn the midst of the pandemic outbreak of corona-virus SARS-CoV-2 therapeutics for disease treatment are still to be tested and the virus-host-interactions are to be elucidated. Drug testing and viral studies are commonly conducted with genetically manipulated cells. In order to find a cell model system without genetic modification we screened human cell lines for two proteins known to facilitate entry of SARS-CoV-2. We confirmed and quantified permissiveness of current cell line infection models, but dismissed a number of receptor-positive cell lines that did not support viral replication. Importantly, ACE2/TMPRSS2 co-expression seems to be necessary for viral entry but is not sufficient to predict permissiveness of various cancer cell lines. Moreover, the expression of specific splice variants and the absence of missense mutations of the host factors might hint on successful infection and virus replication of the cell lines.

scholarly journals Evaluation of Two Extraction Methods for the Analysis of Hydrophilic Low Molecular Weight Compounds from Ganoderma lucidum Spores and Antiproliferative Activity on Human Cell Lines

2020 ◽  
Vol 10 (11) ◽  
pp. 4033
Author(s):  
Maria Michela Salvatore ◽  
Vincenza De Gregorio ◽  
Monica Gallo ◽  
Maria Michela Corsaro ◽  
Angela Casillo ◽  
...  
Keyword(s):  
Molecular Weight ◽  
Cell Lines ◽  
Human Cell ◽  
Ganoderma Lucidum ◽  
Polar Compounds ◽  
Extraction Methods ◽  
Hot Water ◽  
Aqueous Extracts ◽  
Human Cell Lines ◽  
Soxhlet Apparatus

Background: The genus Ganoderma includes about 80 species of mushrooms. Ganoderma lucidum is the best-known fungal species in mycotherapy and likely has the highest number of studies. Numerous bioactive compounds seem to be responsible for its beneficial effects; in particular, triterpenes, peptidoglycans and polysaccharides are the main physiologically active constituents. The aim of the present work is to identify the main bioactive components in aqueous extracts of G. lucidum spores obtained by two different extraction processes. Methods: The spores were at first extracted by a Soxhlet apparatus with n-hexane and the aqueous solutions were submitted to two different procedures: hot water extraction (HWE) and rapid solid-liquid dynamic extraction (RSLDE) using the Naviglio extractor. The extracts were then dialyzed to separate the compounds with higher molecular weight from polar compounds with lower molecular weight. The aqueous extracts and dialyzed fractions were tested on two human cell lines: human colonic epithelial cells (Caco-2) and human colorectal carcinoma cells (HTC-116). Results: GC-MS and NMR data revealed the presence of a mixture of glucose and mannitol in ratio 3.7:1 in the most active fraction. Conclusions: The outside dialysis phase of RSLDE extract seems to be particularly cytotoxic for HTC-116 and, interestingly, solutions with different concentrations of pure mannitol showed cytotoxic activity against this cell line too, although to a lesser extent.

Comparative Toxicity of Bis-pyridinium Acetamide Derivatives in Human Cell Lines and their Acute Toxicity in Swiss Albino Mice

2016 ◽  
Vol 1 (2) ◽  
pp. 149 ◽  
Author(s):  
Devyani Swami ◽  
Nandita Saxena ◽  
Hitendra N Karade ◽  
Pravin Kumar
Keyword(s):  
Cell Lines ◽  
Human Cell ◽  
Oral Route ◽  
Human Cell Lines ◽  
Hep G2 ◽  
Hek 293 ◽  
Routes Of Administration ◽  
Lethal Doses

Having established the antidotal efficacy of 2-(hydroxyimino)-N-(pyridin-3-yl)acetamide (HNK oximes) against Diisopropylphosphorofluoridate (DFP) and sarin poisoning. Toxicity of HNK series and 2-PAM oximes on Human cell lines and Swiss male mice i.e. in vitro and in vivo to reported. Toxicity of the oximes was investigated in Hela, Hep G2 and HEK 293 cell lines and compared with most commonly used 2-PAM. Median lethal doses (LD50) of the oximes (2-PAM, HNK-102, HNK-106, and HNK-111) were also determined following intramuscular, intraperitoneal, intravenous and oral routes of administration. All tested oximes showed no cytotoxic effect on all three cell lines in concentrations up to 0.05 mg/mL. At higher dose (0.5 mg/mL), HNK-102 found to be less toxic thus safer than 2-PAM and other oximes in all the three cell lines. In corroboration with in vitro finding, HNK-102 was found to be least toxic compared to other oximes via intra-peritoneal and intravenous routes of administration. Also, HNK-102 was found to be unequivocally safer compared to that of 2-PAM through i.m. and i.p. routes. For all tested oximes, toxicity following oral route, was found to be lower compared to injections, signifying that these are safer and convenient compounds for administration. These finding also suggested that HNK-102 is safer and better lead as an antidote compared to 2-PAM, against OP intoxicants.

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